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Pronunciation:

(sul fa SAL a zeen)

U.S. Brand Names:

Azulfidine®; Azulfidine® EN-tabs®

Synonyms:

Salicylazosulfapyridine

Generic Available:

Yes: Tablet; excludes delayed release

Canadian Brand Names:

Alti-Sulfasalazine; Salazopyrin®; Salazopyrin En-Tabs®

Use:

Management of ulcerative colitis; enteric coated tablets are also used for rheumatoid arthritis (including juvenile rheumatoid arthritis) in patients who inadequately respond to analgesics and NSAIDs

Use - Unlabeled/Investigational:

Ankylosing spondylitis, collagenous colitis, Crohn's disease, psoriasis, psoriatic arthritis, juvenile chronic arthritis

Pregnancy Risk Factor:

B/D (at term)

Lactation:

Enters breast milk/use caution (AAP recommends use "with caution")

Contraindications:

Hypersensitivity to sulfasalazine, sulfa drugs, salicylates, or any component of the formulation; porphyria; GI or GU obstruction; pregnancy (at term)

Warnings/Precautions:

Use with caution in patients with renal impairment; impaired hepatic function or urinary obstruction, blood dyscrasias, severe allergies or asthma, or G6PD deficiency; may cause folate deficiency (consider providing 1 mg/day folate supplement). Chemical similarities are present among sulfonamides, sulfonylureas, carbonic anhydrase inhibitors, thiazides, and loop diuretics (except ethacrynic acid). Use in patients with sulfonamide allergy is specifically contraindicated in product labeling, however, a risk of cross-reaction exists in patients with allergy to any of these compounds; avoid use when previous reaction has been severe. Safety and efficacy have not been established in children <2 years of age.

Adverse Reactions:

>10%:

Central nervous system: Headache (33%)

Dermatologic: Photosensitivity

Gastrointestinal: Anorexia, nausea, vomiting, diarrhea (33%), gastric distress

Genitourinary: Reversible oligospermia (33%)

<3%:

Dermatologic: Urticaria/pruritus (<3%)

Hematologic: Hemolytic anemia (<3%), Heinz body anemia (<3%)

<0.1%: Alopecia, anaphylaxis, aplastic anemia, ataxia, convulsions, crystalluria, depression, drowsiness, epidermal necrolysis, exfoliative dermatitis, granulocytopenia, hallucinations, hearing loss, hematuria, hepatitis, insomnia, interstitial nephritis, jaundice, leukopenia, Lyell's syndrome, myelodysplastic syndrome, nephropathy (acute), neutropenic enterocolitis, pancreatitis, peripheral neuropathy, photosensitization, rhabdomyolysis, serum sickness-like reactions, skin discoloration, Stevens-Johnson syndrome, thrombocytopenia, thyroid function disturbance, tinnitus, urine discoloration, vasculitis, vertigo

Additional events reported with sulfonamides and/or 5-ASA derivatives: Cholestatic jaundice, eosinophilia pneumonitis, erythema multiforme, fibrosing alveolitis, hepatic necrosis, Kawasaki-like syndrome, SLE-like syndrome, pericarditis, seizure, transverse myelitis

Overdosage/Toxicology:

Symptoms of overdose include drowsiness, dizziness, anorexia, abdominal pain, nausea, vomiting, hemolytic anemia, acidosis, jaundice, fever, and agranulocytosis. The aniline radical is responsible for hematologic toxicity. High volume diuresis may aid in elimination and prevention of renal failure. Leucovorin 5-15 mg/day has been used to speed recovery of bone marrow.

Drug Interactions:

Azathioprine, mercaptopurine, sulfasalazine: May increase the risk of myelosuppression (due to TPMT inhibition).

Cyclosporine concentrations may be decreased; monitor levels and renal function

Digoxin's absorption may be decreased

Folic acid's absorption may be decreased

Hydantoin levels may be increased; monitor levels and adjust as necessary

Hypoglycemics: Increased effect of oral hypoglycemics (rare, but severe); monitor blood sugar

Methenamine: Combination may result in crystalluria; avoid use

Methotrexate-induced bone marrow suppression may be increased

NSAIDs and salicylates: May increase sulfonamide concentrations

PABA (para-aminobenzoic acid - may be found in some vitamin supplements): Interferes with the antibacterial activity of sulfonamides; avoid concurrent use

Sulfinpyrazone: May increase sulfonamide concentrations

Thiazide diuretics: May increase the incidence of thrombocytopenia purpura

Thiopental's effect may be enhanced; monitor for possible dosage reduction

Uricosuric agents: Actions of these agents are potentiated

Warfarin and other oral anticoagulants: Anticoagulant effect may be increased; decrease dose and monitor INR closely

Ethanol/Nutrition/Herb Interactions:

Food: May impair folate absorption.

Herb/Nutraceutical: Avoid dong quai, St John's wort (may also cause photosensitization)

Stability:

Protect from light.

Mechanism of Action:

Acts locally in the colon to decrease the inflammatory response and systemically interferes with secretion by inhibiting prostaglandin synthesis

Pharmacodynamics/Kinetics:

Absorption: 10% to 15% as unchanged drug from small intestine

Distribution: Small amounts enter feces and breast milk

Metabolism: Via colonic intestinal flora to sulfapyridine and 5-aminosalicylic acid (5-ASA); following absorption, sulfapyridine undergoes N-acetylation and ring hydroxylation while 5-ASA undergoes N-acetylation

Half-life elimination: 5.7-10 hours

Excretion: Primarily urine (as unchanged drug, components, and acetylated metabolites)

Dosage:

Oral:

Children 2 years: Ulcerative colitis: Initial: 40-60 mg/kg/day in 3-6 divided doses; maintenance dose: 20-30 mg/kg/day in 4 divided doses

Children 6 years: Juvenile rheumatoid arthritis: Enteric coated tablet: 30-50 mg/kg/day in 2 divided doses; Initial: Begin with ¹/4 to ¹/3 of expected maintenance dose; increase weekly; maximum: 2 g/day typically

Adults:

Ulcerative colitis: Initial: 1 g 3-4 times/day, 2 g/day maintenance in divided doses; may initiate therapy with 0.5-1 g/day

Rheumatoid arthritis: Enteric coated tablet: Initial: 0.5-1 g/day; increase weekly to maintenance dose of 2 g/day in 2 divided doses; maximum: 3 g/day (if response to 2 g/day is inadequate after 12 weeks of treatment)

Dosing interval in renal impairment:

Clcr 10-30 mL/minute: Administer twice daily

Clcr<10 mL/minute: Administer once daily

Dosing adjustment in hepatic impairment: Avoid use

Administration:

GI intolerance is common during the first few days of therapy (administer with meals).

Dietary Considerations:

Since sulfasalazine impairs folate absorption, consider providing 1 mg/day folate supplement.

Patient Education:

Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Take as directed, at regular intervals around-the-clock with food. Do not crush, chew, or dissolve coated tablets. Complete full course of therapy even if you are feeling better. Take a missed dose as soon as possible. If almost time for next dose, skip the missed dose and return to your regular schedule. Do not take a double dose. Maintain adequate hydration (2-3 L/day of fluids) to prevent kidney damage unless instructed to restrict fluid intake. If you have diabetes, monitor glucose levels closely (may cause decreased effect of oral hypoglycemic agents). Orange-yellow color of urine is normal. May cause dizziness or headache (use caution when driving or engaging in tasks requiring alertness until response to drug is known); photosensitivity (use sunblock, wear protective clothing and eyewear, and avoid direct sunlight); or nausea, vomiting, or loss of appetite (small, frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help). Report rash; persistent nausea, vomiting, or diarrhea; opportunistic infection (sore throat, fever, vaginal itching or discharge, unusual bruising or bleeding, fatigue); blood in urine or change in urinary pattern; swelling of face, lips, or tongue, tightness in chest, bad cough, blue skin color, or other persistent adverse effects. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Consult prescriber if breast-feeding.

Nursing Implications:

Drug commonly imparts an orange-yellow discoloration to urine and skin

Dental Health: Effects on Dental Treatment:

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

No information available to require special precautions

Mental Health: Effects on Mental Status:

Dizziness is common; sulfonamides reported to cause restlessness, irritability, depression, euphoria, disorientation, panic, hallucinations, and delusions

Mental Health: Effects on Psychiatric Treatment:

Photosensitivity is common; use caution with concurrent psychotropics; may cause leukopenia; caution with clozapine and carbamazepine

Dosage Forms:

Tablet (Azulfidine®): 500 mg

Tablet, delayed release, enteric coated (Azulfidine® EN-tabs®): 500 mg

International Brand Names:

Alti-Sulfasalazine (CA); Azulfidine® (AR, CL, DE); Azulfidine-EN® (CL); Azulfin® (BR); Colizine® (NZ); Colo-Pleon® (DE); Falazine® (EC); Gastropyrin® (EG, JO, KW, LB); Pleon® (DE); Pyralin EN® (AU); Rosulfant® (CO); Salasopyrin® (BG); Salazidin® (RO); Salazine® (BD); Salazopirina En® (PT); Salazopyrina® (ES); Salazopyrin® (AT, AU, BE, CA, CH, CO, CZ, DK, FI, GB, HK, HR, HU, IE, IL, NO, NZ, PL, RO, SE, TR, YU, ZA); Salazopyrine® (BE, FR, LU, NL); Salazopyrin EN® (HR); Salazopyrin®-EN (IL, IT, RO, SG, TH, TR); Salazopyrin En-Tabs® (CA); Salazopyrin EN-Tabs® (GB, IE, TH); Saridine® (TH); Sazo EN® (IN); Sulazine® (GB); Sulcolon® (ID); Sulfaenterin® (BG); Sulfasalazin® (CZ, HR, PL, SI, YU); Sulfasalazine FNA® (NL); Sulfasalazine® (GB, RU); Sulfasalazin Hexal® (DE); Sulfasalazin-Heyl® (DE); Sulfasalazin medac® (DE); Sulfosalazina® (CO); Sulphasalazine® (CY); Ucine® (GB); Ulcol® (AU)

References

"American Academy of Pediatrics Committee on Drugs. The Transfer of Drugs and Other Chemicals Into Human Milk,"Pediatrics, 2001, 108(3):776-89.

American College of Rheumatology Ad Hoc Committee on Clinical Guidelines, "Guidelines for the Management of Rheumatoid Arthritis,"Arthritis Rheum, 1996, 39(5):713-22.

Ardizzone S and Porro GB, "A Practical Guide to the Management of Distal Ulcerative Colitis,"Drugs, 1998, 55(4):519-42.

Gabay C, DeBandt M, and Palazzo E, "Sulfasalazine-Related Life-threatening Side Effects: Is N-acetylcysteine of Therapeutic Value?"Clin Exp Rheumatol, 1993, 11(4):417-20.

Giannini EH and Cawkwell GD, "Drug Treatment in Children With Juvenile Rheumatoid Arthritis,"Pediatr Clin North Am, 1995, 42(5):1099-125.

Haines JD, Jr, "Hepatotoxicity After Treatment With Sulfasalazine,"Postgrad Med, 1986, 79(6):193-4, 197-8.

Jick H, Myers MW, and Dean AD, "The Risk of Sulfasalazine- and Mesalazine-Associated Blood Disorders,"Pharmacotherapy, 1995, 15(2):176-81.

Jullien D, Wokenstein P, Roupie E, et al, "Toxic Epidermal Necrolysis After Sulfasalazine Treatment of Mild Psoriatic Arthritis: Warning on the Use of Sulfasalazine for a New Indication,"Arthritis Rheum, 1995, 38(4):573.

Kirschner BS, "Inflammatory Bowel Disease in Children,"Pediatr Clin North Am, 1988, 35(1):189-208.

O'Dell JR, "Triple Therapy With Methotrexate, Sulfasalazine, and Hydroxychloroquine in Patients With Rheumatoid Arthritis,"Rheum Dis Clin North Am, 1998, 24(3):465-77.

Peppercorn MA, "Sulfasalazine: Pharmacology, Clinical Use, Toxicity, and Related New Drug Development,"Ann Intern Med, 1984, 101(3):377-86.

van Rossum MA, Fiselier TJ, Franssen MJ, et al, "Sulfasalazine in the Treatment of Juvenile Chronic Arthritis: A Randomized, Double-Blind, Placebo-Controlled, Multicenter Study. Dutch Juvenile Chronic Arthritis Study Group,"Arthritis Rheum, 1998, 41(5):808-16.

Veale DJ, Ho M, and Morley KD, "Sulfasalazine-Induced Lupus in Psoriatic Arthritis,"Br J Rheumatol, 1995, 34(4):383-4.

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